蛇床子素在Caco-2细胞模型中的转运机制研究

 目的 研究蛇床子素在 Caco-2 细胞模型中的转运机制。方法 通过研究蛇床子素在 Caco-2 细胞模型中的转运，考察蛇床子素浓度、PEG600、P-gp抑制剂维拉帕米（verapamil及温度对蛇床子素转运的影响。结果 随着蛇床子素溶液浓度和温度的升高，蛇床子素在Caco-2 细胞中 AP-BL 的转运量增加；PEG600对蛇床子素在 Caco-2 细胞中的 AP-BL 的转运量有显著增加；P-gp 抑制剂维拉帕米对蛇床子素在 Caco-2 细胞中转运的表观通透系数 PAP 和 PBL 无显著影响。结论 蛇床子素表观通透系数 PAP大于10×10-6 cm·s-1，较易被 Caco-2 细胞吸收，但由于3个浓度蛇床子素溶液的PAP 和 PBL比值无明显变化、P-gp 抑制剂对 PAP 和 PBL 无明显影响及转运的活化能较低(17.31 kJ·mol-1，因此，蛇床子素在 Caco-2 细胞模型中的转运机制主要是被动转运。

Study on Transport Mechanisms of Osthol in Caco-2 Cell Model

OBJECTIVE To study the transport mechanisms of osthol by using Caco-2 cell model. METHODS The effect of concentration， PEG600， verapamil(P-gp inhibitorand temperature on transport of osthol in Caco-2 cell model was studied. RESULTS Osthol amount transported in the apical(APto basolateral(BLin Caco-2 cell cell model was increased with loading concentration and temperature. PEG600 enhanced the rate of osthol transport. The PAP and PBL of osthol in Caco-2 model were not affected by verapamil. CONCLUSION The PAP of osthol in Caco-2 model was above 10×10-6 and osthol was absorbed easily by Caco-2 cell. Further， there were no significant differences in the ratios of PBL to PAP at three concentrations. Activation energy was quite moderate at 17.31 kJ·mol-1. The ratio of PBL to PAP of osthol transport were not affected by verapamil， suggesting that the absorption is via passive diffusion.